FTIDC
Based on 1 Customer Validation
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.34%
- No. CAS: 873551-53-2
- Fòrmula: C18H23FN6O
- Peso molecular:358.41
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
mGluR1a 5.8 nM (IC50) |
mGlu5 6200 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
3.1 nM
Compound: 1
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Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
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[PMID: 18849168] |
| CHO | IC50 |
5.8 nM
Compound: 1
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Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
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[PMID: 18849168] |
| CHO | IC50 |
6200 nM
Compound: 1
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Antagonist activity at human mGluR5 expressed in CHO cells assessed as calcium flux by FLIPR assay
Antagonist activity at human mGluR5 expressed in CHO cells assessed as calcium flux by FLIPR assay
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[PMID: 18849168] |
| CHO | IC50 |
5.6 nM
Compound: 1
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Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
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[PMID: 19692242] |
| CHO | IC50 |
>10000 nM
Compound: 1
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Antagonist activity at human mGluR5 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
Antagonist activity at human mGluR5 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
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[PMID: 19692242] |
In Vitro
FTIDC inhibits L-glutamate-induced increases in intracellular Ca2+ concentrations, with IC50 values of 5.8 nM , 5.8 nM , 3.1 nM , 7.7 nM for human mGluR1a, rat mGluR1a, mouse mGluR1a, human mGluR1b in CHO cells, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD1 (ICR) mice of 6-weeks-old[1]
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Dosage:1, 3, 10, and 30 mg/kg
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Administration:I.p. or p.o.
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Result:Reduced the duration of face-washing behavior elicited in a dosedependent manner and was statistically significant at 10 and 30 mg/kg with i.p. and 30 mg/kg with p.o..
Chemical Information
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No. CAS 873551-53-2
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Appearance Solid
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Peso molecular 358.41
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Fòrmula C18H23FN6O
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Color White to light yellow
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SMILES
O=C(N1CC=C(C2=C(C)N(C3=CC=CN=C3F)N=N2)CC1)N(C)C(C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (279.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Suzuki G, et al. Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC). J Pharmacol Exp Ther. 2007 Jun;321(3):1144-53. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7901 mL | 13.9505 mL | 27.9010 mL | 69.7525 mL |
| 5 mM | 0.5580 mL | 2.7901 mL | 5.5802 mL | 13.9505 mL | |
| 10 mM | 0.2790 mL | 1.3951 mL | 2.7901 mL | 6.9753 mL | |
| 15 mM | 0.1860 mL | 0.9300 mL | 1.8601 mL | 4.6502 mL | |
| 20 mM | 0.1395 mL | 0.6975 mL | 1.3951 mL | 3.4876 mL | |
| 25 mM | 0.1116 mL | 0.5580 mL | 1.1160 mL | 2.7901 mL | |
| 30 mM | 0.0930 mL | 0.4650 mL | 0.9300 mL | 2.3251 mL | |
| 40 mM | 0.0698 mL | 0.3488 mL | 0.6975 mL | 1.7438 mL | |
| 50 mM | 0.0558 mL | 0.2790 mL | 0.5580 mL | 1.3951 mL | |
| 60 mM | 0.0465 mL | 0.2325 mL | 0.4650 mL | 1.1625 mL | |
| 80 mM | 0.0349 mL | 0.1744 mL | 0.3488 mL | 0.8719 mL | |
| 100 mM | 0.0279 mL | 0.1395 mL | 0.2790 mL | 0.6975 mL |
FTIDC Related Classifications
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